Abstract
The biological, pharmacological and therapeutic properties of leflunomide in the treatment of rheumatoid arthritis (RA) are reviewed. Leflunomide alone, or in combination with other antirheumatic drugs, is an effective and potent immunosuppressant developed for the treatment of moderate to severe RA.
Leflunomide can be used as a first-line DMARD in patients with RA who cannot tolerate methotrexate or in whom the drug is contraindicated. The addition of leflunomide to methotrexate in patients with RA who do not respond adequately to methotrexate monotherapy can help improve disease activity control.
Leflunomide may be used in combination with anti-TNF and other biological agents, with its effectiveness being comparable to treatment with the combination of methotrexate plus an anti-TNF or another biologic agent. Common adverse events include diarrhoea, nausea, vomiting, rash, alopecia, and minor infections.
Major adverse events include significant lung injury, severe infection, and cytopenia. The risk of adverse events is increased with concurrent medication, particularly methotrexate, alcohol consumption, and a low body weight.